JP2003516346A5 - - Google Patents
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- Publication number
- JP2003516346A5 JP2003516346A5 JP2001543088A JP2001543088A JP2003516346A5 JP 2003516346 A5 JP2003516346 A5 JP 2003516346A5 JP 2001543088 A JP2001543088 A JP 2001543088A JP 2001543088 A JP2001543088 A JP 2001543088A JP 2003516346 A5 JP2003516346 A5 JP 2003516346A5
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- methyl
- amino
- compound according
- phosphinic acid
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 description 10
- 239000003814 drug Substances 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 229910052739 hydrogen Inorganic materials 0.000 description 3
- 239000001257 hydrogen Substances 0.000 description 3
- -1 t-butyl (2R) -2-fluoro-3-hydroxy Propyl Chemical group 0.000 description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- KPELUVFYFBYKOB-QGZVFWFLSA-N (2r)-3-(dibenzylamino)-2-fluoropropan-1-ol Chemical compound C=1C=CC=CC=1CN(C[C@@H](F)CO)CC1=CC=CC=C1 KPELUVFYFBYKOB-QGZVFWFLSA-N 0.000 description 1
- DTXCSCJRPZOOAQ-GSVOUGTGSA-N (2r)-3-amino-2-fluoropropan-1-ol Chemical compound NC[C@@H](F)CO DTXCSCJRPZOOAQ-GSVOUGTGSA-N 0.000 description 1
- KPELUVFYFBYKOB-KRWDZBQOSA-N (2s)-3-(dibenzylamino)-2-fluoropropan-1-ol Chemical compound C=1C=CC=CC=1CN(C[C@H](F)CO)CC1=CC=CC=C1 KPELUVFYFBYKOB-KRWDZBQOSA-N 0.000 description 1
- DTXCSCJRPZOOAQ-VKHMYHEASA-N (2s)-3-amino-2-fluoropropan-1-ol Chemical compound NC[C@H](F)CO DTXCSCJRPZOOAQ-VKHMYHEASA-N 0.000 description 1
- QSEZFOAWAVHOBH-UHFFFAOYSA-N (3-amino-2-fluoropropyl)-methylphosphinic acid Chemical compound CP(O)(=O)CC(F)CN QSEZFOAWAVHOBH-UHFFFAOYSA-N 0.000 description 1
- HYTZHDBUDDPKNK-UHFFFAOYSA-N (4-amino-3-fluorobutan-2-yl)-methylphosphinic acid Chemical compound CP(=O)(O)C(C)C(F)CN HYTZHDBUDDPKNK-UHFFFAOYSA-N 0.000 description 1
- 0 *C(C(*)N*)C(*)P(*)(O)=O Chemical compound *C(C(*)N*)C(*)P(*)(O)=O 0.000 description 1
- AYRXSQGCNIIFNH-UHFFFAOYSA-N 3-[ethoxy(methyl)phosphoryl]-2-fluorobutanamide Chemical compound CCOP(C)(=O)C(C)C(F)C(N)=O AYRXSQGCNIIFNH-UHFFFAOYSA-N 0.000 description 1
- XDZUTZCCXHGOLU-UHFFFAOYSA-N 3-[ethoxy(methyl)phosphoryl]-2-fluoropropanamide Chemical compound CCOP(C)(=O)CC(F)C(N)=O XDZUTZCCXHGOLU-UHFFFAOYSA-N 0.000 description 1
- RYZXCMIPPGQXGJ-UHFFFAOYSA-N 3-iodopropyl carbamate Chemical compound NC(=O)OCCCI RYZXCMIPPGQXGJ-UHFFFAOYSA-N 0.000 description 1
- 208000022497 Cocaine-Related disease Diseases 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- 208000031361 Hiccup Diseases 0.000 description 1
- 208000002193 Pain Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- WVTGPBOMAQLPCP-GSVOUGTGSA-O [(2r)-3-amino-2-fluoropropyl]-hydroxy-oxophosphanium Chemical compound NC[C@@H](F)C[P+](O)=O WVTGPBOMAQLPCP-GSVOUGTGSA-O 0.000 description 1
- QSEZFOAWAVHOBH-SCSAIBSYSA-N [(2r)-3-amino-2-fluoropropyl]-methylphosphinic acid Chemical compound CP(O)(=O)C[C@H](F)CN QSEZFOAWAVHOBH-SCSAIBSYSA-N 0.000 description 1
- WVTGPBOMAQLPCP-VKHMYHEASA-O [(2s)-3-amino-2-fluoropropyl]-hydroxy-oxophosphanium Chemical compound NC[C@H](F)C[P+](O)=O WVTGPBOMAQLPCP-VKHMYHEASA-O 0.000 description 1
- QSEZFOAWAVHOBH-BYPYZUCNSA-N [(2s)-3-amino-2-fluoropropyl]-methylphosphinic acid Chemical compound CP(O)(=O)C[C@@H](F)CN QSEZFOAWAVHOBH-BYPYZUCNSA-N 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 208000006673 asthma Diseases 0.000 description 1
- 201000006145 cocaine dependence Diseases 0.000 description 1
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 206010013663 drug dependence Diseases 0.000 description 1
- 201000006549 dyspepsia Diseases 0.000 description 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 1
- GPVFBPLHTWJJFY-UHFFFAOYSA-N ethyl 3-[ethoxy(methyl)phosphoryl]-2-fluoropropanoate Chemical compound CCOC(=O)C(F)CP(C)(=O)OCC GPVFBPLHTWJJFY-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 description 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 description 1
- 208000002551 irritable bowel syndrome Diseases 0.000 description 1
- 210000000111 lower esophageal sphincter Anatomy 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- OBKSTEOVEUUBBH-KRWDZBQOSA-N methyl (2s)-3-(dibenzylamino)-2-fluoropropanoate Chemical compound C=1C=CC=CC=1CN(C[C@H](F)C(=O)OC)CC1=CC=CC=C1 OBKSTEOVEUUBBH-KRWDZBQOSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- LFGREXWGYUGZLY-UHFFFAOYSA-N phosphoryl Chemical group [P]=O LFGREXWGYUGZLY-UHFFFAOYSA-N 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000020341 sensory perception of pain Effects 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE9904507A SE9904507D0 (sv) | 1999-12-09 | 1999-12-09 | New compounds |
| SE9904507-2 | 1999-12-09 | ||
| PCT/SE2000/002427 WO2001041743A1 (en) | 1999-12-09 | 2000-12-04 | New (aminopropyl)methylphosphinic acids |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2003516346A JP2003516346A (ja) | 2003-05-13 |
| JP2003516346A5 true JP2003516346A5 (enrdf_load_stackoverflow) | 2008-01-17 |
Family
ID=20418062
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001543088A Pending JP2003516346A (ja) | 1999-12-09 | 2000-12-04 | 新規な（アミノプロピル）メチルホスフィン酸 |
Country Status (26)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7319095B2 (en) * | 1999-12-09 | 2008-01-15 | Astrazeneca Ab | Use of GABAB receptor agonists |
| SE9904508D0 (sv) * | 1999-12-09 | 1999-12-09 | Astra Ab | New compounds |
| TW200407110A (en) | 2001-11-23 | 2004-05-16 | Astrazeneca Ab | New use for the treatment of gastroesophageal reflux disease |
| SE0201939D0 (sv) * | 2002-06-20 | 2002-06-20 | Astrazeneca Ab | New combination |
| SE0201940D0 (sv) * | 2002-06-20 | 2002-06-20 | Astrazeneca Ab | New combination II |
| DE10305463A1 (de) * | 2003-02-04 | 2004-08-12 | Schering Ag | Enantiomerenreines (4S,8S)- und (4R,8R)-4-p-Nitrobenzyl-8-methyl-3,6,9-triza-3N,6N,9N-tricarboxymethyl-1,11-undecandisäure und deren Abkömmlinge, Verfahren zu deren Herstellung und Verwendung zur Herstellung pharmazeutischer Mittel |
| SE0401653D0 (sv) | 2004-06-24 | 2004-06-24 | Astrazeneca Ab | New compounds |
| SE0402462D0 (sv) * | 2004-10-08 | 2004-10-08 | Astrazeneca Ab | New process |
| US7812026B2 (en) | 2005-12-23 | 2010-10-12 | Astrazeneca Ab | Imidazole derivatives having a positive allosteric GABAB receptor modulator effect and methods of use |
| CN101341130A (zh) | 2005-12-23 | 2009-01-07 | 阿斯利康(瑞典)有限公司 | 用于治疗胃肠障碍的咪唑衍生物 |
| CN101675064B (zh) | 2007-05-04 | 2012-11-14 | 阿斯利康(瑞典)有限公司 | 由胺和氧化胺引发的合成烷基次膦酸的方法 |
| WO2009014491A1 (en) * | 2007-07-25 | 2009-01-29 | Astrazeneca Ab | The use of (3-amino-2-fluoropropyl) phosphinic acid for treatment of nerd |
| US20110054216A1 (en) * | 2007-12-21 | 2011-03-03 | Hassan Abbasi | Novel process for making (2r)-(3-amino-2-fluoropropyl)phosphinic acid form a |
| US20110034420A1 (en) * | 2007-12-21 | 2011-02-10 | Ida Hoyer | Novel crystalline form b of (2r)-(3-amino-2-fluoropropyl)phosphinic acid |
| JP2011026260A (ja) * | 2009-07-28 | 2011-02-10 | Central Glass Co Ltd | ３位に脱離基を有する２−フルオロプロピルアミン保護体または該アミンｎ−アルキル保護体 |
| WO2011113904A1 (en) | 2010-03-17 | 2011-09-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Medicaments for the prevention and treatment of a disease associated with retinal ganglion cell degeneration |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH449046A (de) | 1963-07-09 | 1967-12-31 | Ciba Geigy | Verfahren zur Herstellung neuer Aminosäuren |
| SU643510A1 (ru) * | 1975-04-11 | 1979-01-25 | Предприятие П/Я А-7815 | Способ получени о-аминофениларилфосфиновых кислот |
| SU589756A1 (ru) * | 1976-01-23 | 1982-10-07 | Институт Органической Химии Ан Усср | Способ получени солей перфторалкилфосфиновых кислот |
| GB8425872D0 (en) | 1984-10-12 | 1984-11-21 | Ciba Geigy Ag | Chemical compounds |
| WO1987004077A1 (en) | 1986-01-03 | 1987-07-16 | The University Of Melbourne | Gastro-oesophageal reflux composition |
| GB8820266D0 (en) | 1988-08-26 | 1988-09-28 | Smith Kline French Lab | Compounds |
| US5567840A (en) * | 1989-05-13 | 1996-10-22 | Ciba-Geigy Corporation | Substituted aminoalkylphosphinic acids |
| GB8911017D0 (en) * | 1989-05-13 | 1989-06-28 | Ciba Geigy Ag | Substituted aminoalkylphosphinic acids |
| US5281747A (en) * | 1989-05-13 | 1994-01-25 | Ciba-Geigy Corporation | Substituted aminoalkylphosphinic acids |
| FR2663934B1 (fr) | 1990-06-27 | 1994-06-03 | Adir | Nouveaux derives de l'acide 4 - amino butyrique, leur procede de preparation et les preparations pharmaceutiques qui les contiennent. |
| FR2722192A1 (fr) | 1994-07-06 | 1996-01-12 | Adir | Nouveaux derives de l'acide 4-amino butyrique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| GB9420784D0 (en) | 1994-10-14 | 1994-11-30 | Glaxo Group Ltd | Medicaments |
| SE9603408D0 (sv) | 1996-09-18 | 1996-09-18 | Astra Ab | Medical use |
-
1999
- 1999-12-09 SE SE9904507A patent/SE9904507D0/xx unknown
-
2000
- 2000-04-12 UA UA2002064506A patent/UA73149C2/uk unknown
- 2000-11-27 TW TW089125146A patent/TWI225415B/zh not_active IP Right Cessation
- 2000-12-04 CA CA002393510A patent/CA2393510A1/en not_active Abandoned
- 2000-12-04 KR KR1020027007356A patent/KR100752010B1/ko not_active Expired - Fee Related
- 2000-12-04 BR BR0016291-4A patent/BR0016291A/pt not_active Application Discontinuation
- 2000-12-04 CZ CZ20021984A patent/CZ20021984A3/cs unknown
- 2000-12-04 HU HU0300386A patent/HUP0300386A3/hu unknown
- 2000-12-04 AU AU22412/01A patent/AU780259B2/en not_active Ceased
- 2000-12-04 PL PL00357115A patent/PL357115A1/xx not_active IP Right Cessation
- 2000-12-04 EP EP00986117A patent/EP1239843A1/en not_active Withdrawn
- 2000-12-04 WO PCT/SE2000/002427 patent/WO2001041743A1/en active IP Right Grant
- 2000-12-04 EE EEP200200287A patent/EE200200287A/xx unknown
- 2000-12-04 MX MXPA02005537A patent/MXPA02005537A/es active IP Right Grant
- 2000-12-04 SK SK763-2002A patent/SK7632002A3/sk not_active Application Discontinuation
- 2000-12-04 RU RU2002113916/04A patent/RU2267495C2/ru not_active Application Discontinuation
- 2000-12-04 CN CNB008169063A patent/CN1200713C/zh not_active Expired - Fee Related
- 2000-12-04 IL IL15009000A patent/IL150090A0/xx active IP Right Grant
- 2000-12-04 NZ NZ519377A patent/NZ519377A/en unknown
- 2000-12-04 US US09/786,220 patent/US6596711B1/en not_active Expired - Fee Related
- 2000-12-04 JP JP2001543088A patent/JP2003516346A/ja active Pending
- 2000-12-05 AR ARP000106429A patent/AR033350A1/es unknown
- 2000-12-06 CO CO00093168A patent/CO5261538A1/es not_active Application Discontinuation
-
2002
- 2002-05-23 ZA ZA200204122A patent/ZA200204122B/xx unknown
- 2002-06-06 IL IL150090A patent/IL150090A/en not_active IP Right Cessation
- 2002-06-06 IS IS6409A patent/IS6409A/is unknown
- 2002-06-07 NO NO20022729A patent/NO20022729L/no not_active Application Discontinuation